In-Vivo Evaluation of Some Novel Chromen- 2 One Based on Pharmacological Activity of Antipsychotic Drug

Most neuroleptics block the emesis hyper activity and aggression induced by apomorphine and other dopaminergic agonists. In higher doses, most neoroleptics induce characteristic cataleptic immobility that allows the animal to be placed in abnormal postures that persists, the aim of this project work was to carry out preliminary pharmacological screening of 2-[(4-methyl-2-oxo-2H-chromen-7-yl) oxy-(aryl)] acetamide. preliminary pharmacological screening of the synthesized compounds for the antipsychotic activity. The screening was limited to in vivo models only. The synthesized compounds were converted to their hydrochloride salts in order to make them water-soluble. These hydrochloride salts were used for the pharmacological testing purpose. The experiments were performed on Swiss albino mice (male) and the route of administration was intra peritoneal

STUDY OF INFLUENCE OF FORMULATION AND PROCESS VARIABLES ON ENTRAPMENT EFFICIENCY AND PARTICLE SIZE OF FLOATING MICRO BALLOONS OF DIPYRIDAMOLE BY DOE

Objective: In the current research work, dipyridamole, a BCS class–II drug, was aimed to be formulated as floating controlled release microballoons using ethyl cellulose as polymer and span 80 as surfactant to improve the gastric retention of drug as the multi-particulate dosage forms have tremendous advantages over single unit dosage forms. Methods: Microballoons were prepared by the emulsion solvent evaporation method. Prepared microballoons were characterized for entrapment efficiency, particle size, floating behavior and drug release studies. The study of effect of various formulation and process parameters like surfactant concentration, solvent volume, the volume of internal phase, polymer concentration, rotation speed on the drug entrapment efficiency and particle size of the microballoons were carried by using Box–Benhken to optimize the formulated microballoons. Results: The smallest particle size of the microballoons was found to be 205.9 µm in the F32 formulation. The highest drug entrapment efficiency was found to be 93.4% in the F34 formulation. Buoyancy studies showed all the formulations have good floating characteristics that lasted for a minimum of 24 h. The maximum yield of microballoons was found in the F7 formulation with 91.8% yield. The final results were statistically treated using ANOVA and were found to be significant (p value<0.05). Conclusion: Thus, the obtained results and their statistical interpretations indicated floating microballoons of dipyridamole were formulated effectively

Formulation and Evaluation of Liquid Loaded Tablets Containing Docetaxel-Self Nano Emulsifying Drug Delivery Systems

Purpose: To prepare and characterize tablets loaded with self-nanoemulsifying drug delivery system (SNEDDS) containing docetaxel (DTL).Method: SNEDDS of docetaxel were prepared using various oils, surfactants, co-surfactant and solvents to improve the dissolution rate and bioavailability of the poorly water-soluble chemotherapeutic agent. The SNEDDS components were preliminarily screened for the solubility of the drug in various vehicles, miscibility of excipients, rate of emulsification and ternary phase diagrams. The tablets were prepared by direct compression process with a porous carrier, magnesium alumino-metasilicate, and subsequently loaded with SNEDDS by a simple absorption method. The tablets were then characterized for physical parameters, including tablet hardness, weight variation, disintegration, drug content and invitro drug release.Results: Cremophor-EL, polysorbate-80 and dehydrated alcohol mixture in the ratio 85:10:5 yielded docetaxel SNEDDS with droplet size of 12.16 nm and polydispersity (PDI) of 0.039. Tablets with high porosity suitable for loading with SNEDDS and containg the super-disintegrants, crosscarmellose sodium and sodium starch glycolate, in a concentration of 3, 4 and 5 %, achieved complete dissolution of docetaxel from the tablets. In vitro release of docetaxel from SNEDDS and the tablets was similar (p < 0.05).Conclusion: SNEDDS of docetaxel is a promising approach to achieving a solid dosage form of the liquid-loaded drug delivery systems for enhancing the solubility and dissolution rate of the drug, and hence also its bioavailability.Keywords: Docetaxel, Drug carrier, SNEDDS, Self-nanoemulsifying, Solubility, Drug release, Anicancer, Surfactant, Co-surfactan

BIOAVAILABILITY ENHANCEMENT BY FLOATING MICROBALLOONS OF DIPYRIDAMOLE AND CLOPIDOGREL: IN VIVO PHARMACOKINETIC STUDY

Objective: In vivo pharmacokinetic studies of clopidogrel and dipyridamole floating microballoons to check their bioavailability enhancement. Methods: The bioanalytical method development was carried by using HPLC with column Poroshell 120 EC-C 18; 4.6x100 mm. The in vivo pharmacokinetic studies were performed in Wistar male rats and the obtained data from the pharmacokinetic parameters were analyzed using PK Solver software. Results: The developed bioanalytical method was found to be linear in the concentration range of 1-100 ng/ml for clopidogrel bisulfate and 0.02-4µg/ml for dipyridamole with correlation coefficient of 0.9993 and 0.9987 respectively. The study results showed that the method was simple, linear, accurate and precise. The in vivo studies indicated that the AUC was found to be increased by 33.3% and 154.5% for clopidogrel and dipyridamole micro balloons, respectively, when compared to their pure drugs. Conclusion: The bioanalytical methods development and their validation parameters indicated that the methods are accurate, precise and linear in the studied range of concentrations. In vivo test results infer to the effective, sustained release of both the drugs when formulated as micro balloons and increase in the absorption, thereby enhancing the bioavailability of the drugs. The pharmacokinetic studies also confirmed the increase in the mean residence time of the drugs when formulated as floating microballoons

FORMULATION AND EVALUATION OF ESOMEPRAZOLE FAST DISSOLVING BUCCAL FILMS

Objective: The present study deals with the formulation and evaluation of fast dissolving buccal films for effective treatment option in the gastroesophageal reflux disease.Methods: Esomeprazole fast dissolving buccal films are a convenient formulation of which can be taken with or without water. In the present investigation, polyvinyl alcohol and polyvinylpyrrolidone were used as film-forming agents and polyethylene glycol 400 is taken as plasticizer. Solvent evaporation method was used for the preparation of fast dissolving buccal films.Results: The films were prepared and evaluated for film thickness, folding endurance, dispersion test, drug content, and dissolution. The in vitro dissolution studies were carried out using simulated salivary fluid (pH 6.8 phosphate buffer).Conclusion: Among all the formulations, Formulation E7 was released up to 99.6% of the drug from the film within 5 min of time which exhibits faster absorption and also shows desirable characteristics of the film. The drug-excipient interaction studies WERE carried out by Fourier-transform infrared studies, differential scanning calorimetry analysis-X-diffraction studies, and scanning electron microscopic studies and the results revealed that there were no major interactions between the drugs and excipients used for the preparation of films

METHOD DEVELOPMENT AND VALIDATION FOR THE ESTIMATION OF ENTECAVIR IN BULK AND PHARMACEUTICAL DOSAGE FORMS BY RP-HPLC

Objective: The objective and purpose of the analysis have sensibly assessed by selecting of a rapid and sensitive RP-HPLC method for Entecavir in bulk and pharmaceutical dosage form by using the most commonly employed C-18column with UV detection.Methods: In estimation by RP-HPLC method Agilent 1120 compact LC system with variable programmable UV detector and Rheodyne injector with 20 µl fixed loop was used for the chromatographic separation. The mode of operation was isocratic with the components of a solution consisting of methanol: acetonitrile(70:30v/v) and triethanolamine (2-4drops)at the flow rate of 1.2 ml/min and run time was 10 min. Forced degradation studies were conducted to evaluate the stability and specificity of the method along with the validation parameters.Results: Validation parameters of HPLC were found at a detection wavelength of 255 nm. Linearity was observed with the concentration range (Beer's law range) 20-100µg/ml with R2=0.9991. Robustness with detection wavelengths 253 and 257 nm with a flow rate of 1 ml/min and 1.4 ml/min showed good results. The retention time of the drug was 2.64 min and assay showed 98.1%.Conclusion: The proposed RP-HPLC method was validated as per the ICH Q2B Guidelines, and was found to be applicable for routine quantitative analysis of Entecavir by RP-HPLC using UV detector in pharmaceutical dosage forms. The results of linearity, precision, accuracy and specificity, were proved, that does not exceed certain specified limits. The method provides selective quantification with no interference from other formulation excipients. The proposed method was highly sensitive, reproducible, reliable, robust and specific. Therefore, this method is a simple, rapid analysis may actually be more desirable than a more complicated and time-consuming process. The degradation studies at various stress conditions like thermal and hydrolytic, drug gets degraded at a temperature of 80 °c and refluxing with water at 70 °c for 24hours.Â

SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF TELMISARTAN BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING KOLLIDON VA 64 AS CARRIER

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Telmisartan solid dispersions were prepared by solvent evaporation technique using Kollidon VA64 as binder and solubility enhancer, Crospovidone as disintegrant and ethanol was used as the solvent. Telmisartan pellets were prepared by dissolving telmisartan, kollidonVA64, Crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. All the formulations were further evaluated for physicochemical parameters such as particle size, friability, angle of repose and drug content. In vitro dissolution studies were carried out in pH 7.5 phosphate buffer by using USP apparatus II. Results: It was observed that the dissolution rate of the solid dispersion formulation TSD5 showed a better dissolution rate to the extent of 1.113 folds and 1.979 folds when compared to a marketed formulation and pure drug, respectively. Similarly, the formulation TPL3containing 1:3 ratio of Telmisartan to Kollidon VA64 showed an improved dissolution rate to the extent of 1.150 folds and 2.045 folds when compared to the marketed formulation and pure drug, respectively. Majority of the formulations displayed first-order release kinetics and were found to be linear with R2 values in the range of 0.905 to 0.994. FTIR analysis and DSC analysis revealed that there was no major interaction between the drug and the excipients used in the design of the formulation. SEM analysis was performed for solid dispersions, pellet formulations and its polymers to determine the surface characteristics. Conclusion: From the present study, it was observed that the solubility of Telmisartan was enhanced by Kollidon VA 64 in pellet formulations when compared to solid dispersions

Mayer-Rokitansky-Kuster-Hauser syndrome with gonadohypoplasia:a rare case report

MRKH (Mayer Rokitansky Kuster Hauser) syndrome is a congenital abnormality seen in one out of 5,000 women characterized by the agenesis of the vagina, cervix, and uterus. It is also associated with kidney, bone and hearing difficulties. The ovaries are present with a normal function similar to that of a healthy reproductive woman’s by producing eggs and female hormones. Chromosomes are the normal 46xx female karyotype. We report this rare syndrome in a 26–year-old female where she had presented with complaints of absence of uterus with the absence of left kidney. She didn’t attain menarchy, secondary sexual characters are well developed. Small right ovarian follicular cyst with a rim of ovarian tissue was observed. She had undergone vaginoplasty